Aceclofenac, also named 2-[2-[2-[(2,6-dichlorophenyl)amino]phenyl]acetyl]oxyacetic acid (CAS RN: 89796-99-6) is a nonsteroidal anti-inflammatory agent, with remarkable anti-inflammatory, analgesic and antipyretic properties. The usual dosage of aceclofenac, normally presented in its acid form, is of two daily doses of 100 mg.
Cyclobenzaprine, also named 3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine is a tricyclic muscle relaxant used in the treatment of muscular spasm related with painful musculoskeletal conditions. Usual dosages of cyclobenzaprine (normally presented in the form of hydrochloride salt) are of 3 daily dosages of 5 mg or 10 mg, and the main side effects of the drug are related to drowsiness and dizziness.
Although there are several references about the combined use of cyclobenzaprine with nonsteroidal anti-inflammatory drugs, results of clinical controlled studies are non-conclusive about the real benefit of the use of said association, mainly when the potential side effects of cyclobenzaprine are considered.
Aiming for the obtainment of products with a suitable safety and efficacy profile, as well as easiness of administration for the treatment of diseases which have concomitancy between inflammatory, painful spasm and excessive muscular contraction components, the present inventors noted that association of cyclobenzaprine with aceclofenac can be specially interesting, due to the high analgesic and anti-inflammatory strength of aceclofenac associated to its favorable safety profile, its fast action outset and its prolonged effect.
In a complementary aspect, the present inventors noted that, due to chemical interactions, it is particularly interesting the vehiculation of cyclobenzaprine and aceclofenac in pharmaceutical products that avoid contact between the two active ingredients and/or prevent such interactions.
Within the best knowledge of the present inventors, there is not, in the present state of the art, any publication concerning the efficacy and safety of the specific association of aceclofenac with cyclobenzaprine, neither about the chemical interaction between said active ingredients.